SML3445

VT104

≥98% (HPLC)

• 别名: (S)-N-(l-(Pyridin-2-yl)ethyl)-5-(4-(trifluoromethyl)phenyl)-2-naphthamide, N-[(1S)-1-(2-Pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide, VT-104
• 经验公式（希尔记法）: C₂₅H₁₉F₃N₂O
• CAS号: 2417718-25-1
• 分子量: 420.43
• 分類程式碼代碼: 12352200
• NACRES: NA.21

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 2 mg/mL, clear
• 儲存溫度: 2-8°C
• SMILES 字串: FC(F)(C1=CC=C(C2=CC=CC3=CC(C(N[C@H](C4=NC=CC=C4)C)=O)=CC=C23)C=C1)F
• InChI: 1S/C25H19F3N2O/c1-16(23-7-2-3-14-29-23)30-24(31)19-10-13-22-18(15-19)5-4-6-21(22)17-8-11-20(12-9-17)25(26,27)28/h2-16H,1H3,(H,30,31)/t16-/m0/s1
• InChI 密鑰: AAZUPSFRSHFTGV-INIZCTEOSA-N

说明

生化／生理作用

Orally available pan-TEAD auto-palmitoylation inhibitor with anti-proliferation efficacy against mesothelioma with NF2 defect in cultures and in vivo.

VT104 is an orally available pan-TEAD auto-palmitoylation inhibitor (3 μM; using TEAD isotype-overexpressing HEK293T) that blocks TEAD-mediated gene transcription (IC50 = 10.4 nM) by preventing its association with YAP/TAZ. VT104 selectively inhibits the proliferation of mesothelioma cultures with NF2 mutation (NCI-H2051 IC50 = 31.6 nM), deletion (NCI-H2373 IC50 = 25.6 nM) or deficiency (NCI-H226 IC50 = 16.1 nM), but not those with wild-type NF2. Oral administration is efficacious against human mesothelioma NCI-H226 tumor growth in mice in vivo (1-3 mg/kg/day).

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable